| Tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate | IC50 | 39.1 [1], 56.7 [2], 69.0 [3], 81.0 [4] |
| Tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate | Ki | 6.6 [1], 8.9 [2] |
| Molibresib | IC50 | 42.4 [1], 160.0 [2], 390.0 [3], 400.0 [4] |
| Molibresib | Ki | 30.3 [1], 53.9 [2] |
| Birabresib | IC50 | 21.0 [1], 38.5 [2], 92.0 [3] |
| Birabresib | Ki | 4.0 [1], 10.7 [2] |
| I-Bet151 (gsk1210151A) | IC50 | 250.0 [1], 251.19 [2] |
| I-Bet151 (gsk1210151A) | Ki | 7.2 [1], 22.3 [2] |
| 4-[(2s,4r)-1-Acetyl-4-[(4-Chlorophenyl)amino]-2-Methyl-1,2,3,4-Tetrahydroquinolin-6-Yl]benzoic Acid | IC50 | 0.25 [1], 0.63 [2], 2.0 [3], 199.53 [4] |
| Apabetalone | IC50 | 203.0 [1], 510.0 [2], 3962.0 [3] |
| Tert-butyl 2-[7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate | IC50 | 19.1 [1], 39.0 [2], 59.0 [3] |
| Benzyl [(4r)-1-Methyl-6-Phenyl-4h-[1,2,4]triazolo[4,3-A][1,4]benzodiazepin-4-Yl]carbamate | IC50 | 28.4 [1], 220.0 [2], 350.0 [3] |
| 4-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-pyridin-2-ylbenzenesulfonamide | Ki | 100.0 [1], 140.0 [2] |
| 8-[[(3R,4R)-3-[(1,1-Dioxothian-4-yl)methoxy]piperidin-4-yl]amino]-3-methyl-5-(5-methylpyridin-3-yl)-1H-1,7-naphthyridin-2-one | IC50 | 50118.72 [1] |
| 4-[(2-Amino-3-chloro-4-hydroxy-5-methylphenyl)diazenyl]-N-pyridin-2-ylbenzenesulfonamide | Ki | 240.0 [1], 320.0 [2] |
| 1-[1-(Pyridin-2-Yl)indolizin-3-Yl]ethan-1-One | IC50 | 2500.0 [1], 6300.0 [2] |
| 4-[1-(3-Cyclopropyl-5-methyl-1H-pyrazol-4-yl)-8-methoxy-5H-pyrido[4,3-b]indol-7-yl]-3,5-dimethyl-1,2-oxazole | Ki | 3.2 [1], 7.3 [2] |
| 5-(5-Methoxypyridin-3-Yl)-3-Methyl-8-[(Piperidin-4-Yl)amino]-1,2-Dihydro-1,7-Naphthyridin-2-One | IC50 | 6309.57 [1], 19952.62 [2] |
| 3-Methyl-5-(5-methylpyridin-3-yl)-8-(piperidin-4-ylamino)-1H-1,7-naphthyridin-2-one | IC50 | 7943.28 [1], 19952.62 [2] |
| 3-[(4-Chlorophenyl)methyl]-7-Ethyl-Purine-2,6-Dione | IC50 | 1800.0 [1] |
| 4-[1-(5-Ethyl-3-phenyl-1H-pyrazol-4-yl)-8-methoxy-5H-pyrido[4,3-b]indol-7-yl]-3,5-dimethyl-1,2-oxazole | Ki | 9.4 [1], 10.4 [2] |
| 8-[[(3R,4R)-3-[(1,1-Dioxothian-4-yl)methoxy]-1-methylpiperidin-4-yl]amino]-3-methyl-5-(5-methylpyridin-3-yl)-1H-1,7-naphthyridin-2-one | IC50 | 50118.72 [1] |
| 3-Butyl-7-ethylpurine-2,6-dione | IC50 | 4800.0 [1], 5800.0 [2] |
| 4-[(5-Cyclopropyl-2-ethylpyrazol-3-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-N-methyl-9H-pyrimido[4,5-b]indole-2-carboxamide | IC50 | 6.6 [1] |
| 4-[(5-Cyclopropyl-2-ethylpyrazol-3-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-N-methyl-9H-pyrimido[4,5-b]indole-2-carboxamide | Ki | 0.21 [1] |
| 4-[(E)-(4-Hydroxy-3,5-Dimethylphenyl)diazenyl]-N-(Pyridin-2-Yl)benzenesulfonamide | Ki | 1640.0 [1], 2480.0 [2] |
| 4-[(E)-(2-Amino-4-Hydroxy-3,5-Dimethylphenyl)diazenyl]-N-(Pyridin-2-Yl)benzenesulfonamide | Ki | 220.0 [1], 290.0 [2] |
| 5-(4-Hydroxy-3,5-dimethylphenyl)-11-methyl-8-thia-4,6,11-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),5-trien-3-one | IC50 | 100000.0 [1] |
| 4-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-cyclopentylbenzenesulfonamide | IC50 | 2241.0 [1], 2493.0 [2] |
| 6-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-3,4-dihydro-1H-quinolin-2-one | IC50 | 2193.0 [1], 2275.0 [2] |
| 5-[(2S)-1-Acetyl-2-cyclopropyl-4-[[2-(hydroxymethyl)phenyl]methyl]-2,3-dihydroquinoxalin-6-yl]pyrimidine-2-carboxamide | IC50 | 31.62 [1], 794.33 [2] |
| 1-[(2S)-2-Cyclopropyl-4-[[2-(hydroxymethyl)phenyl]methyl]-6-(1,2,3,6-tetrahydropyridin-4-yl)-2,3-dihydroquinoxalin-1-yl]ethanone | IC50 | 50.12 [1], 1258.93 [2] |
| 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-6-methoxy-N-methyl-9H-pyrimido[4,5-b]indole-2-carboxamide | IC50 | 294.0 [1] |
| 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-6-methoxy-N-methyl-9H-pyrimido[4,5-b]indole-2-carboxamide | Ki | 42.4 [1] |
| N-Cyclopentyl-5-(3,5-dimethyl-1,2-oxazol-4-yl)-2-methoxybenzenesulfonamide | IC50 | 200.0 [1], 1000.0 [2] |
| N-Cyclopentyl-5-(3,5-Dimethylisoxazol-4-Yl)-2-Methylbenzenesulfonamide | IC50 | 250.0 [1], 500.0 [2] |
| 4-[1-(3,5-Diethyl-1H-pyrazol-4-yl)-8-methoxy-5H-pyrido[4,3-b]indol-7-yl]-3,5-dimethyl-1,2-oxazole | Ki | 4.2 [1], 12.9 [2] |
| 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one | IC50 | 13700.0 [1] |
| 2-Piperazinyl-8-phenyl-4H-1-benzopyran-4-one | IC50 | 11500.0 [1] |
| Mivebresib | Ki | 12.2 [1] |
| Benzyl N-(1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl)carbamate | IC50 | 630.96 [1] |
| 4-[(2-Tert-Butylphenyl)amino]-7-(3,5-Dimethyl-1,2-Oxazol-4-Yl)quinoline-3-Carboxylic Acid | IC50 | 501.19 [1] |
| 5-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-tert-butylpyridine-3-sulfonamide | IC50 | 10000.0 [1] |
| 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-(pyridin-2-ylmethyl)-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 501.19 [1] |
| 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-phenylethyl]-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 199.53 [1] |
| 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-1-(2-fluorophenyl)-8-methoxy-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 630.96 [1] |
| 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1S)-1-phenylethyl]-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 630.96 [1] |
| 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-4-(2-fluoroanilino)quinoline-3-carboxamide | IC50 | 3162.28 [1] |
| 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-4-(2-fluoroanilino)-6-methoxyquinoline-3-carboxamide | IC50 | 316.23 [1] |
| 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-6-methoxy-4-(quinolin-8-ylamino)quinoline-3-carboxamide | IC50 | 501.19 [1] |
| 1-(2-Tert-butylphenyl)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 398.11 [1] |
| 4-(Cyclohexylamino)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxyquinoline-3-carboxamide | IC50 | 501.19 [1] |
| 1-Benzyl-7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 251.19 [1] |
| N-[3-(3-Methyl-4-Oxo-4,5,6,7-Tetrahydro-2h-Isoindol-1-Yl)-4-Phenoxyphenyl]methanesulfonamide | Ki | 35.0 [1] |
| 1-[2-(2,4-Difluorophenoxy)-5-methylsulfonylphenyl]-3-methyl-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-4-one | Ki | 110.0 [1] |
| N'-(1,1-Dioxothian-4-yl)-5-ethyl-4-oxo-7-[3-(trifluoromethyl)phenyl]thieno[3,2-c]pyridine-2-carboximidamide | IC50 | 50118.72 [1] |
| 1-[(2S,4R)-4-Anilino-2-methyl-6-phenyl-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 501.19 [1] |
| 4-[(2S,4R)-1-Acetyl-4-anilino-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzonitrile | IC50 | 794.33 [1] |
| 1-[(2S,4R)-4-Anilino-2-methyl-6-[4-(trifluoromethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 1258.93 [1] |
| 1-[(2S,4R)-4-Anilino-6-(4-methoxyphenyl)-2-methyl-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 630.96 [1] |
| 1-[(2S,4R)-4-Anilino-6-[4-(hydroxymethyl)phenyl]-2-methyl-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 501.19 [1] |
| 1-[(2S,4R)-4-Anilino-2-methyl-6-[4-(morpholin-4-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 630.96 [1] |
| 1-[(2S,4R)-4-Anilino-2-methyl-6-[3-(piperidin-1-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 398.11 [1] |
| 1-[(2R,4S)-4-Anilino-2-methyl-6-[4-(piperidin-1-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 25118.86 [1] |
| Methyl 4-[(2S,4R)-1-acetyl-4-(4-tert-butylanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoate | IC50 | 501.19 [1] |
| 4-[(2S,4R)-1-Acetyl-2-methyl-4-(4-methylsulfonylanilino)-3,4-dihydro-2H-quinolin-6-yl]benzoic acid | IC50 | 316.23 [1] |
| Methyl 4-[(2S,4R)-1-acetyl-2-methyl-4-(4-methylsulfonylanilino)-3,4-dihydro-2H-quinolin-6-yl]benzoate | IC50 | 501.19 [1] |
| Methyl 4-[(2S,4R)-1-acetyl-4-(4-fluoroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoate | IC50 | 1000.0 [1] |
| 4-[(2S,4R)-1-Acetyl-4-(3-fluoroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzonitrile | IC50 | 794.33 [1] |
| 4-[(2S,4R)-1-Acetyl-4-(3-methoxyanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzonitrile | IC50 | 794.33 [1] |
| 4-[(2S,4R)-1-Acetyl-4-(3-methoxyanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoic acid | IC50 | 501.19 [1] |
| 4-[(2S,4R)-1-Acetyl-4-(2-methoxyanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoic acid | IC50 | 501.19 [1] |
| 1-[(2S,4R)-4-(4-Chloroanilino)-2-methyl-6-[4-(piperidin-1-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 1258.93 [1] |
| 3-[(2S,4R)-1-Acetyl-4-(4-chloroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoic acid | IC50 | 501.19 [1] |
| Methyl 3-[(2S,4R)-1-acetyl-4-(4-chloroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoate | IC50 | 1000.0 [1] |
| 1-[(2S,4R)-4-(4-Chloroanilino)-2-methyl-6-(2-methylphenyl)-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 2511.89 [1] |
| 1-[(4R)-4-Anilino-6-(4-methoxyphenyl)-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 1584.89 [1] |
| 7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 25.0 [1] |
| Methyl 7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxylate | IC50 | 18.0 [1] |
| 7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxylic acid | IC50 | 16.0 [1] |
| 7-(4-Chlorophenyl)-1-methyl-9-(1H-pyrazol-5-yl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 10.0 [1] |
| 5-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]pyrimidin-2-amine | IC50 | 14.0 [1] |
| (5S)-7-(4-Chlorophenyl)-1,5-dimethyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 13.0 [1] |
| (5R)-7-(4-Chlorophenyl)-1,5-dimethyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 11.0 [1] |
| N-Benzhydryl-7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 39.0 [1] |
| 7-(4-Chlorophenyl)-N-[(1S)-1-(4-fluorophenyl)ethyl]-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 23.0 [1] |
| 2-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-5-yl]ethanol | IC50 | 44.0 [1] |
| [7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]methanol | IC50 | 36.0 [1] |
| 7-(4-Chlorophenyl)-1-methyl-9-(6-methylpyridin-3-yl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 10.0 [1] |
| 1-Methyl-7-phenyl-5H-triazolo[1,5-d][1,4]benzodiazepin-6-one | IC50 | 10000.0 [1] |
| 5-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]pyridin-2-amine | IC50 | 9.0 [1] |
| 1-Methyl-7-phenyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 19.0 [1] |
| N-(Benzenesulfonyl)-7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 21.0 [1] |
| 7-(4-Chlorophenyl)-1-methyl-N-phenyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 14.0 [1] |
| N-Benzyl-7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 21.0 [1] |
| 7-(4-Chlorophenyl)-1-methyl-N-[(1S)-1-phenylethyl]-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 12.0 [1] |
| 7-(4-Chlorophenyl)-1-methyl-N-[(1R)-1-phenylethyl]-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 13.0 [1] |
| 8-[(5-Amino-1H-1,2,4-triazol-3-yl)sulfanylmethyl]-3-[(4-chlorophenyl)methyl]-7-ethylpurine-2,6-dione | IC50 | 31700.0 [1] |
| 7-(4-Chlorophenyl)-1-methyl-9-(pyrazol-1-ylmethyl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 52.0 [1] |
| 1-Methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-amine | IC50 | 12589.25 [1] |